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Supercritical Antisolvent Precipitation of Corticosteroids/β-Cyclodextrin Inclusion Complexes
Stefania Mottola1,2, Iolanda De Marco1,2
1Department of Industrial Engineering, University of Salerno, Via Giovanni Paolo II 132, 84084 Fisciano, SA, Italy.
Polymers
|January 11, 2024
Summary
Supercritical antisolvent precipitation created corticosteroid-beta-cyclodextrin inclusion complexes, significantly enhancing the dissolution of dexamethasone and prednisolone. These novel microparticles demonstrate a threefold faster release rate compared to pure drugs.
Area of Science:
- Pharmaceutical Technology
- Materials Science
- Drug Delivery Systems
Background:
- Poor water solubility of corticosteroids like dexamethasone (DEX) and prednisolone (PRED) limits their therapeutic efficacy.
- Beta-cyclodextrin (β-CD) is a common host molecule for forming inclusion complexes to improve drug solubility and dissolution.
- Supercritical antisolvent (SAS) precipitation is a green technology for particle engineering.
Purpose of the Study:
- To prepare and characterize corticosteroid-β-CD inclusion complexes using SAS precipitation.
- To enhance the dissolution rate and modify the particle characteristics of DEX and PRED.
- To investigate the influence of process parameters on complex formation and drug release.
Main Methods:
- Preparation of corticosteroid-β-CD inclusion complexes via SAS precipitation with varying concentrations, pressures, and molar ratios.
- Characterization of microparticle size using dynamic light scattering.
- Confirmation of inclusion complex formation using Job's method.
- In vitro drug release studies and kinetic analysis using the Weibull model.
Main Results:
- Optimized SAS conditions (40 °C, 120 bar, equimolar ratio, 20 mg/mL DMSO) yielded microparticles of DEX (0.197 ± 0.180 μm) and PRED (0.131 ± 0.070 μm).
- Job's method confirmed a 1:1 mol/mol inclusion complex stoichiometry for both corticosteroids.
- Obtained powders exhibited a threefold faster release rate compared to pure DEX and PRED.
- Weibull model best described the release kinetics, indicating a combined Fickian diffusion and controlled release mechanism.
Conclusions:
- SAS precipitation is effective for preparing corticosteroid-β-CD inclusion complexes with improved dissolution profiles.
- The optimized microparticles offer a promising approach for enhancing the bioavailability of poorly soluble corticosteroids.
- The combined release mechanism suggests a complex interplay of diffusion and matrix erosion/relaxation.
Keywords:
SAS micronizationcontrolled releasecorticosteroidinclusion complexsupercritical antisolventsupercritical carbon dioxideβ-cyclodextrinMore Related Videos
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